U.S. Patent 10,898,477 Madhavi et. Al January 26, 2021

Nutraceuticals having sustained release for improved bioavailability and method of production

The present disclosure describes economical processes to improve the bioavailability of nutraceuticals by formulations that induce micronization and sustained release. The inventive process can be used to increase the solubility and bioavailability of lipophilic and moderately water-soluble nutraceuticals by combining excipients that increase the solubility and induce sustained release of the active compounds. The inventive process also can be used to increase the residence time of highly water-soluble nutraceuticals that are metabolized and eliminated quickly from the body, consequently increasing the therapeutic potential. The disclosed formulations advantageously are freely flowing powders that can be used to formulate with other ingredients into tablets, capsules, or the like; or used as bulk powders.

We claim:

1. A method for making a water dispersible nutraceutical powder composition comprising the steps of: (a) blending a lipophilic nutraceutical with a mixture of a lipid and a surfactant, the mixture heated to 70.degree. to produce a first non-aqueous mixture, wherein (i) the lipophilic nutraceutical is selected from the group consisting of a carotenoid, a carotenoid ester, a curcuminoid, policosanol, silymarin, baicalein, quercetin, a plant sterol, a vitamin, alpha lipoic acid, a sesquiterpene lactone, and mixtures thereof; (ii) the lipid is selected from the group consisting of a vegetable oil, a medium chain triglyceride, an isopropyl or an ethyl ester of a fatty acid, and mixtures thereof; and (iii) the surfactant is selected from the group consisting of a non-ionic polysorbate material, a polyglycerol ester of a fatty acid having a hydrophilic-lipophilic balance value between about 8 and 18, and mixtures thereof; (b) blending the first non-aqueous mixture with a polymer selected from the group consisting of carboxymethyl cellulose, ethyl cellulose, hydroxypropyl methylcellulose, alginic add sodium salt, a dextrin, carrageenan, a cyclodextrin, and mixtures thereof to produce a second non-aqueous mixture; (c) cooling the second non-aqueous mixture to about room temperature; and (d) blending the cooled second non-aqueous mixture with an excipient selected from the group consisting of microcrystalline cellulose, silica, maltodextrin, potato starch, bamboo silica, rice flower, and mixtures thereof to form a micronized water dispersible lipophilic nutraceutical powder.